THIQ 40( THIQ40 )

Catalog No. M12721 CAS No. 1799430-91-3

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Product Name

THIQ 40
Note

Research use only, not for human use.
Brief Description

THIQ 40 (THIQ40) is a potent, orally available ERα antagonist and selective estrogen receptor degrader (SERD) with IC50 of 17 nM (ERα binding) and 30 nM (ERα transcription), IC50 of 0.9 nM (ERα degradation).
Description

THIQ 40 (THIQ40) is a potent, orally available ERα antagonist and selective estrogen receptor degrader (SERD) with IC50 of 17 nM (ERα binding) and 30 nM (ERα transcription), IC50 of 0.9 nM (ERα degradation); potently inhibits insulin driven proliferation in MCF-7 cells with IC50 of 2.1 nM, downregulate ERα protein levels and inhibit MCF-7 proliferation in an estradiol-independent manner; demonstrated SERD activity at tolerated and efficacious exposures in vivo.
In Vitro

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In Vivo

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Synonyms

THIQ40
Pathway

Endocrinology/Hormones
Target

Estrogen Receptor/ERR
Recptor

Estrogen Receptor/ERR
Research Area

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Indication

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CAS Number

1799430-91-3
Formula Weight

427.544
Molecular Formula

C28H29NO3
Purity

>98% (HPLC)
Solubility

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SMILES

CC(C)C1=CC=C(C=C1)N2CCC3=C(C2(C)C4=CC=C(C=C4)C=CC(=O)O)C=CC(=C3)O
Chemical Name

(E)-3-(4-(6-Hydroxy-2-(4-isopropylphenyl)-1-methyl-1,2,3,4-tetrahydroisoquinolin-1-yl)phenyl)acrylic Acid

1. Burks HE, et al. J Med Chem. 2017 Apr 13;60(7):2790-2818.

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